CN105392473A - External-use composition producing foamed state upon use - Google Patents
External-use composition producing foamed state upon use Download PDFInfo
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- CN105392473A CN105392473A CN201480037345.2A CN201480037345A CN105392473A CN 105392473 A CN105392473 A CN 105392473A CN 201480037345 A CN201480037345 A CN 201480037345A CN 105392473 A CN105392473 A CN 105392473A
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K31/355—Tocopherols, e.g. vitamin E
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- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
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- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
- A61K31/727—Heparin; Heparan
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
- A61K9/122—Foams; Dry foams
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
- B65B—MACHINES, APPARATUS OR DEVICES FOR, OR METHODS OF, PACKAGING ARTICLES OR MATERIALS; UNPACKING
- B65B3/00—Packaging plastic material, semiliquids, liquids or mixed solids and liquids, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans, or jars
- B65B3/04—Methods of, or means for, filling the material into the containers or receptacles
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
- B65D—CONTAINERS FOR STORAGE OR TRANSPORT OF ARTICLES OR MATERIALS, e.g. BAGS, BARRELS, BOTTLES, BOXES, CANS, CARTONS, CRATES, DRUMS, JARS, TANKS, HOPPERS, FORWARDING CONTAINERS; ACCESSORIES, CLOSURES, OR FITTINGS THEREFOR; PACKAGING ELEMENTS; PACKAGES
- B65D83/00—Containers or packages with special means for dispensing contents
- B65D83/14—Containers or packages with special means for dispensing contents for delivery of liquid or semi-liquid contents by internal gaseous pressure, i.e. aerosol containers comprising propellant for a product delivered by a propellant
- B65D83/75—Aerosol containers not provided for in groups B65D83/16 - B65D83/74
- B65D83/752—Aerosol containers not provided for in groups B65D83/16 - B65D83/74 characterised by the use of specific products or propellants
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Provided is a means for heightening the retention of an active ingredient in a composition for a pump foamer. Provided is an external-use composition that contains 1) N-alkyl-2-pyrrolidone and/or a diester carbonate and 2) a surfactant, and that is characterized by having a foamed state upon use.
Description
Technical field
The present invention relates to topical composition, more specifically, when relating to use, produce the topical composition of foam state.
Background technology
External medicine preparation can be divided into the preparation of 5 types substantially: lotion preparation, ointment formulation, cream preparation, atomizing aerosol preparation and foaming aerosol agent formulation.Among those, atomizing aerosol preparation and foaming aerosol agent formulation receive much concern, because these preparations can by evenly and be applied to region, affected part widely and reduce physical stimulation to this region (such as, see, patent document 1) simultaneously.But on the other hand, becoming known for spraying the gas composition of aerosol itself likely stimulates to skin (such as, see, patent document 2).There is a kind of method avoiding this problem, wherein use pump type foam maker (pumpfoamer) to form aerosol (such as foam), and without filling-foam gas.With regard to the foam formed with regard to using pump type foam maker, the ability of this formation of foam can reduce due to solvent composition or polyhydric alcohol usually, and the prescription only having extremely limited kinds is suitable for.In other words, need to research and develop a kind of method that raising is retained in the amount for the effective ingredient in the compositions of pump type foam maker always.
On the other hand, solvent such as propylene carbonate has been used for making aerosol foam (see, such as, patent document 3 and patent document 4), but they never use in the compositions for pump type foam maker.This is true lower than the formation of foam ability of formation of foam gas for this formation of foam ability being considered to due to pump type foam maker.
Topical composition, it contains: 1) N-alkyl-2-Pyrrolidone and/or carbonic diester; With 2) surfactant; Wherein compositions is foam state and for pump type foam maker, it is unknown completely in use.
Prior art file
Patent document
Patent document 1:JP2007-314494A
Patent document 2:JP10-158122A
Patent document 3:JP2006-137722A
Patent document 4:JP08-291050A
Summary of the invention
Technical problem
The present invention makes under these circumstances, and an object of the present invention is to provide a kind of method that raising is retained in the amount for the effective ingredient in the compositions of pump type foam maker.
The solution of problem
In view of the foregoing, the present inventor furthers investigate with a kind of method finding raising to be retained in the amount for the effective ingredient in the compositions of pump type foam maker, and, finally, invented a kind of topical composition, it contains: 1) N-alkyl-2-Pyrrolidone and/or carbonic diester; With 2) surfactant; Wherein compositions is foam state and for pump type foam maker, said composition has above-mentioned character, thus realizes the present invention in use.Therefore, the present invention is as follows.
<1> topical composition, it comprises: 1) N-alkyl-2-Pyrrolidone and/or carbonic diester; With 2) surfactant, wherein said composition is foam state in use.
The topical composition of <2> according to <1>, it comprises: 1) effective ingredient; 2) N-alkyl-2-Pyrrolidone and/or carbonic diester; With 3) surfactant, wherein said compositions is foam state in use.
The topical composition of <3> according to <2>, wherein said effective ingredient comprises and is selected from following one or more: vitamin A and derivant, vitamin D and derivant thereof, vitamin E and derivant, immunosuppressant, antibiotic, antifungal, antiinflammatory, glucocorticoid, heparin and heparinoid.
The topical composition of <4> according to any one of <1> to <3>, wherein said N-alkyl-2-Pyrrolidone comprises and is selected from following one or more: METHYLPYRROLIDONE, N-ethyl-2-pyrrolidone, N-propyl group-2-Pyrrolidone and N-butyl-2-Pyrrolidone.
The topical composition of <5> according to any one of <1> to <4>, wherein said carbonic diester is propylene carbonate.
The topical composition of <6> according to any one of <1> to <5>, wherein said surfactant comprises and is selected from following one or more: optionally add polyoxyethylated glycerine monofatty ester; The fatty acid ester of polyglycereol; The polyoxyethylated sorbitan fatty acid ester of optional interpolation; Polyoxyethylated alkyl ether or alkene ether; Fatty diglycollic amide; The polyoxyethylene castor oil be optionally hydrogenated.
The topical composition of <7> according to any one of <1> to <6>, it comprises the alcohol being not less than 10 quality %.
The topical composition of <8> according to <7>, it comprises the glycerol being not less than 15 quality %.
The topical composition of <9> according to any one of <1> to <8>, it forms foam with pump type foam maker in use.
Topical composition according to any one of <2> to <9> is filled to the medicine prepared in pump type foam maker by <10>.
The beneficial effect of the invention
According to the present invention, a kind of raising can be provided to be retained in the method for the amount for the effective ingredient in the compositions of pump type foam maker.
The description of embodiment
<1> is as the effective ingredient of the main component of externally-applied medicinal composition of the present invention
A mode of topical composition of the present invention is externally-applied medicinal composition, and it comprises: 1) effective ingredient; 2) N-alkyl-2-Pyrrolidone and/or carbonic diester; With 3) surfactant; Said composition is foam state in use.
The effective ingredient as main component is contained by the pharmaceutical pack be filled to by topical composition of the present invention prepared by pump type foam maker.The effective ingredient that can be used for topical composition of the present invention does not limit, as long as this composition is defined as the effective ingredient of medicine by medicine thing method, and preferably can be selected from following instance: vitamin A and derivant thereof, such as retinol, retinoic acid and tocoretinol; Vitamin D and derivant thereof, such as vitamin D
2, vitamin D
3, Maxacalcitol and adapalene; Vitamin E and derivant thereof, such as tocopherol and tretinointocoferil; Immunosuppressant, such as cyclosporin and tacrolimus; Antibiotic, such as achromycin, tetracycline, gentamycin, chloromycetin, benzylpenicillin, polymyxin and methanesulfonic acid polymyxin; Antifungal, such as butenafine, terbinafine, bifonazole, lanoconazole and luliconazole; Antiinflammatory, such as indomethacin, ketoprofen, ketotifen, furan of receiving draw coffee (Nalfurafine) and suprofen; Glucocorticoid, such as hydrocortisone, prednisolone, Dexamethasone valerate and mometasone furoate; And heparin and heparinoid, such as chrondroitin-4-sulfate, chrondroitin-6-sulfate, dermatan acid and Keratin are sour.The content of this effective ingredient does not limit, as long as it meets the normally used content of each composition, and this content is preferably the about 0.001-10% of described topical composition total amount in mass, more preferably from about 0.005-5%.
Topical composition of the present invention can be applicable to as doctor's the effective elements of the medicine and the disease of onset with reference to conventional formulation and dosage.
<2> is as the N-alkyl-2-Pyrrolidone of the main component of topical composition of the present invention and carbonic diester
Topical composition of the present invention comprises N-alkyl-2-Pyrrolidone and/or carbonic diester.In formation of the present invention, these compositions have makes effective ingredient dissolve and can not destroy the effect that pump type foam maker forms the ability of foam.Only a kind of composition can be used, or use the combination of two or more compositions.For the performance of above-mentioned effect, the total content of described composition is preferably the about 0.5-10% of described topical composition total amount in mass, more preferably 1-5%.
When content is too small, possibly cannot give full play to the effect that this effective ingredient dissolves, and when content is excessive, formation of foam ability may be destroyed.The preferred embodiment of the alkyl in N-alkyl-2-Pyrrolidone comprises methyl, ethyl, propyl group and butyl.This alkyl is particularly preferably methyl or ethyl.
For carbonic diester, the cyclic diester of dihydroxylic alcohols or the diester of two monohydric alcohols can be adopted.The preferred embodiment of this carbonic diester comprises the pungent diester of ethylene carbonate, propylene carbonate and carbonic acid.
<3> is as the surfactant of the main component of topical composition of the present invention
Topical composition of the present invention contains the surfactant as main component.The example of this surfactant comprises non-ionic surface active agent, anion surfactant, cationic surfactant and amphoteric surfactant.Among those, non-ionic surface active agent is particularly preferred.Especially, described surfactant is preferably selected from: the polyoxyethylated glycerine monofatty ester of optional interpolation; The fatty acid ester of polyglycereol; The polyoxyethylated sorbitan fatty acid ester of optional interpolation; Polyoxyethylated alkyl ether or alkene ether; Fatty diglycollic amide; The polyoxyethylene castor oil be optionally hydrogenated.
Polyoxyethylated average addition molal quantity is preferably 5-25.
The average addition molal quantity of polyglycereol is preferably 2-10.
The average carbon atom number forming the fatty acid of glycerine monofatty ester, polyglyceryl fatty acid ester or sorbitan fatty acid ester is preferably 6-18, is more preferably 6-16.
The average carbon atom number of the alkyl or alkenyl in polyoxyethylated alkyl ether or alkene ether is preferably 10-16.
The average carbon atom number forming the fatty acid of fatty diglycollic amide is preferably 10-18, is particularly preferably 10-14.
The particularly preferred mode of surfactant is the mode using following combination: a) polyoxyethylene (average addition molal quantity, 6-10) fatty acid (average carbon atom number, 6-14) monoglyceride and/or fatty diglycollic amide; And b) polyoxyethylene (average addition molal quantity, 8-25) alkyl ether and/or polyoxyethylene (average addition molal quantity, 20-80) castor oil hydrogenated.
In this case, from the view point of stablizing this dissolution system, a) polyoxyethylene (average addition molal quantity, 6-10) fatty acid (average carbon atom number, 6-14) monoglyceride and/or fatty diglycollic amide and b) polyoxyethylene (average addition molal quantity, mass ratio 8-25) between alkyl ether and/or polyoxyethylene (average addition molal quantity, 20-80) castor oil hydrogenated is particularly preferably 1:4-1:1.Because topical composition of the present invention is administered to the impaired skin of possibility; and can use under the condition of not carrying out cleaning treatment; therefore said composition is preferably substantially free of anion surfactant, cationic surfactant or amphoteric surfactant, or the amino acid pattern of acidylate (aminoacid-based) surfactant.
The content of the surfactant in topical composition of the present invention is preferably the 0.1-10% of described topical composition total amount in mass, more preferably 0.5-7%.
In topical composition of the present invention, count in mass ratio, 2) N-alkyl-2-Pyrrolidone and/or carbonic diester and 3) ratio between surfactant is generally 20:1-1:20, preferred 15:1-1:15, more preferably 10:1-1:10.By using this surfactant, the topical composition with good formation of foam ability and excellent stability can be provided.In addition, under this content ratio, the dissolubility of this effective ingredient increases.
Topical composition of the present invention comprises described main component, and is soluble preparation.Said composition uses with external form.Topical composition of the present invention, also can containing any formulation ingredients being generally used for pharmaceutical composition except containing this main component.The preferred embodiment of this composition comprises oil and wax, such as macadimia nut oil, American Avocado Tree oil, Semen Maydis oil, olive oil, Oleum Brassicae campestris, Oleum sesami, Oleum Ricini, safflower oil, Oleum Gossypii semen, simmondsia oil, Oleum Cocois, Petiolus Trachycarpi oil, liquid lanolin, hydrogenated palm oil, hydrogenated oil and fat, Japan wax, castor oil hydrogenated, Cera Flava, candelilla wax, Brazil wax, East Asia Fructus Ligustri Lucidi wax (ibotawax), lanoline, reduction lanoline, hard lanoline and jojoba wax; Hydrocarbon, such as liquid paraffin, squalane, pristane, ceresine, paraffin, ceresin, vaseline and microwax; Higher fatty acids, such as oleic acid, isostearic acid, lauric acid, myristic acid, Palmic acid, stearic acid, behenic acid and undecylenic acid; Higher alcohol, such as spermol, stearyl alcohol, isooctadecanol, behenyl alcohol, octyldodecanol, myristyl alcohol and cetostearyl alcohol; Synthesis ester oil, such as isooctyl acid cetyl ester, isopropyl myristate, isostearic acid hexyl decyl ester, ethylene glycol bisthioglycolate-2-ethylhexanoate, neopentyl glycol dicaprate, glycerol two-2-heptyl undecylate, glycerol three-2-ethylhexanoate, trimethylolpropane tris-2-ethylhexanoate, trimethylolpropane tris isostearate and pentane erithritol four-2-ethylhexanoate; Chain polysiloxanes, such as dimethyl polysiloxane, methyl phenyl silicone and diphenylpolysiloxane; Cyclic polysiloxanes, such as octamethylcy-clotetrasiloxane, decamethylcyclopentasiloxane and ten dimethyl cyclohexane siloxanes; Oil, such as silicone oil, comprise the polysiloxanes of modification, such as, and the polysiloxanes that amido modified polysiloxanes, the polysiloxanes of alkyl modified and fluorine are modified; Polyhydric alcohol, such as Polyethylene Glycol, glycerol, 1,3-butanediol, erithritol, Sorbitol, xylitol, maltose alcohol, propylene glycol, dipropylene glycol, two glycerol, isoprenediol (isopreneglycol), 1,2-pentanediol, 2,4-hexanediol, 1,2-hexanediol and 1,2-ethohexadiol; Moisturizing ingredient, such as lactic acid and sodium lactate; Powder, such as Muscovitum, Talcum, Kaolin, artificial mica, calcium carbonate, magnesium carbonate, silica anhydride (silicon dioxide), aluminium oxide and barium sulfate, they optionally carry out surface treatment; Inorganic pigment, such as red iron oxide, yellow iron oxide, black iron oxide, cobalt oxide, dark purple, Prussian blue, titanium oxide and zinc oxide, they optionally carry out surface treatment; Margarita, such as mica titanium, guanin and bismuth oxychloride, they optionally carry out surface treatment; Organic dyestuff, such as No. 202, redness, No. 228, redness, No. 226, redness, No. 4, yellow, No. 404, blueness, Sunset Yellow FCF, No. 505, redness, No. 230, redness, redness No. 223, orange No. 201, No. 213, redness, No. 204, yellow, No. 203, yellow, No. 1, blueness, No. 201, green, No. 201, purple and No. 204, redness, it can be pigementation dyestuff (lakedye); Organic dust, such as polyethylene powders, poly-(methyl methacrylate), nylon powder and organopolysiloxane elastomers; UV absorbent, such as based on the UV absorbent of para-amino benzoic acid, based on the UV absorbent of anthranilic acid, based on salicylic UV absorbent, the UV absorbent based on cinnamic acid, the UV absorbent based on benzophenone, UV absorbent based on sugar, 2-(2 '-hydroxyl-5 '-tertiary octyl phenyl) benzotriazole and 4-methoxyl group-4 '-tert-butyl group DBM; Lower alcohol, such as ethanol and isopropyl alcohol; Antimicrobial, such as phenyl phenol; Antibacterial, such as methyl parahydroxybenzoate; Substrate, such as Polyethylene Glycol; PH adjusting agent, such as sodium hydroxide; Plasticizer; And solvent, such as crotamiton and benzylalcohol.
Particularly preferably the example of component comprises the ester of medium-chain fatty acid, such as medium chain triglyceride; Do not belong to the dibasic acid ester of carbonic diester, such as diethylene adipate, diisopropyl adipate and ethyl sebacate; And plasticizer, such as triethyl citrate, diethylene glycol monoethyl ether and Sunsoft 767.These improve the dissolubility of described effective ingredient.By mass, the content of each these compositions is preferably 1-15% relative to the total amount of described topical composition.
Other preferred embodiments of this solvent comprise alcohol.This alcohol is preferably the combination of ethanol and polyhydric alcohol.Content ratio (mass ratio) between them is preferably 1:4 to 4:1.
The preferred embodiment of described polyhydric alcohol comprises 1,3 butylene glycol, isoprene (3-methyl isophthalic acid, 3-butanediol), 1,2-pentanediol, Polyethylene Glycol, propylene glycol, polypropylene glycol and glycerol.By mass, the content of this alcohol is preferably not less than 10% relative to the total amount of described topical composition, is especially preferably 20-60%.The scheme wherein comprising the glycerol being not less than 15 quality % is preferred, is more preferably 20 quality %.Usually, at the content of alcohol more than the situation of 10 quality %, especially at the content of glycerol more than the situation of 15 quality %, it is difficult for bubbling with pump type foam maker.The present invention is by overcoming this problem with nonionic surfactant combinations.
Conventionally, described main component and any composition can be processed into topical composition by soluble form, and by being filled in pump type foam maker by resulting composition, said composition are processed into medicine.
This pump type foam maker does not limit, as long as it makes said composition bubble with soluble form.Can make to apply some make up and usually adopt in medicine those.This pump type foam maker is preferably used as externally-applied medicinal composition.
That is, external of the present invention (medicine) compositions is the compositions for external (medicine) compositions of the foam state produced by pump type foam maker.
Because the topical composition obtained thus is soluble preparation, therefore this effective ingredient is evenly dissolved in wherein, and said composition can use with form of foam.Therefore, said composition can be coated on affected part glibly and can not stimulate to this region, and this effective ingredient can be uniformly distributed in whole affected part.In this way, the effect of this effective ingredient can be given full play to.
Embodiment
The present invention is further described in more detail hereinafter by embodiment.
< embodiment 1>
According to prescription described below, prepare externally-applied medicinal composition 1 of the present invention.That is, by formulation ingredients 80 DEG C of heating, stirring and dissolving, and then stir make it to be cooled to room temperature, obtain externally-applied medicinal composition 1 of the present invention.Said composition is filled to pump type foam maker (being manufactured by DaiwaCan company), obtains external used medicine 1 of the present invention.It discharges fine foam.
[table 1]
Table 1
< comparative example 1>
METHYLPYRROLIDONE in externally-applied medicinal composition 1 is replaced to diisopropyl adipate, makes comparative externally-applied medicinal composition 1.Said composition is filled to pump type foam maker, and discharges from this pump type foam maker.As a result, almost can not find foam, and said composition is discharged as liquid.
< embodiment 2>
According to prescription described below, prepare externally-applied medicinal composition 2 by the mode identical with embodiment 1.The compositions of preparation is filled in pump type foam maker, obtains external used medicine 2 of the present invention.It discharges fine foam.
[table 2]
Table 2
< embodiment 3>
According to prescription described below, prepare externally-applied medicinal composition 3 by the mode identical with embodiment 1.The compositions of preparation is filled to pump type foam maker to obtain external used medicine 3 of the present invention.It discharges fine foam.
[table 3]
Table 3
< embodiment 4>
According to prescription hereinafter described, prepare externally-applied medicinal composition 4 by the mode identical with embodiment 1.The compositions of preparation is filled to pump type foam maker, obtains external used medicine 4 of the present invention.It discharges fine foam.
[table 4]
Table 4
< embodiment 5>
According to prescription described below, prepare externally-applied medicinal composition 5 by the mode identical with embodiment 1.The compositions of preparation is filled to pump type foam maker, obtains external used medicine 5 of the present invention.It discharges fine foam.
[table 5]
Table 5
< embodiment 6-10>
According to hereinafter described prescription, prepare the externally-applied medicinal composition of externally-applied medicinal composition 6-10 and comparative example 2 and 3 in the same manner as example 1.Each compositions is filled to pump type foam maker, obtains the external used medicine of external used medicine 6-10 of the present invention and comparative example 2 and 3.In table 6, the content of each formulation ingredients represents with the quality % of relative externally-applied medicinal composition total amount.External used medicine of the present invention discharges fine foam.The external used medicine of comparative example 2 cannot uniform dissolution.The external used medicine of comparative example 2 and 3 produces foam hardly and discharges with liquid.
[table 6]
Table 6
< embodiment 11 and 12>
According to hereinafter described prescription, prepare externally-applied medicinal composition 11 and 12.That is, each composition of each composition of each composition of (A), (B), (C) is incorporated in 80 DEG C of heating for dissolving with each composition of (D) is mixed respectively, then makes gained mixture be cooled to room temperature.In the mixture (A) add to the mixture of the mixture of (B), (C) and the mixture of (D) successively, obtain externally-applied medicinal composition 11 and 12 of the present invention.Each externally-applied medicinal composition 11 and 12 is filled to pump type foam maker, obtains external used medicine 11 and 12 of the present invention.In table 7, content the representing with the quality % of the total amount relative to externally-applied medicinal composition of each formulation ingredients.External used medicine of the present invention discharges fine foam.
[table 7]
Table 7
< embodiment 13>
< method of testing >
In each 200-mL high type glass beaker, place the externally-applied medicinal composition 8 or 10 of embodiment 8 or 10 of 100g, or the externally-applied medicinal composition of comparative example 2 or 3, and each compositions homo-mixer is stirred with 3000rpm within 1 minute, make it to bubble.Afterwards, said composition is left standstill 2 minutes, until the boundary line of foam and solution centre becomes clear.The height of this foam uses slide calliper rule to measure.Result is as shown in table 8.
Externally-applied medicinal composition 8 and 10 produces highly higher foam, and shows good foaming.On the other hand, the externally-applied medicinal composition of comparative example 1 and 2 produces highly lower foam, and demonstrates poor foaming.
[table 8]
Table 8
< embodiment 14-18>
According to hereinafter described prescription, prepare externally-applied medicinal composition 14-18 in the same manner as example 1, and the externally-applied medicinal composition of comparative example 4 and 5.Each compositions is filled to pump type foam maker, obtains the external used medicine of external used medicine 14-18 of the present invention and comparative example 4 and 5.In table 9, the content of each formulation ingredients represents with the quality % of the total amount relative to externally-applied medicinal composition.External used medicine 14-18 of the present invention discharges fine foam.The external used medicine of comparative example 4 and 5 shows poor foaming, and compositions is discharged as the liquid of low formation of foam ability.
[table 9]
Table 9
< embodiment 19>
< method of testing >
For the externally-applied medicinal composition of each externally-applied medicinal composition 14-17 and comparative example 4 and 5, the method for testing according to embodiment 13 measures the height of this foam.Result is as shown in table 10.Externally-applied medicinal composition 14-17 produces highly higher foam, and demonstrates good foaming.On the other hand, the externally-applied medicinal composition of comparative example 4 and 5 produces highly lower foam, and shows poor foaming.
[table 10]
Table 10
< embodiment 20-22>
According to hereinafter described prescription, prepare topical composition 20-22 in the same manner as example 1.Each compositions is filled to pump type foam maker, obtains external preparation 20-22 of the present invention.External preparation of the present invention discharges fine foam.
[table 11]
Table 11
[table 12]
Table 12
[table 13]
Table 13
Commercial Application
The present invention can be used for medicine.
Claims (10)
1. topical composition, it comprises:
1) N-alkyl-2-Pyrrolidone and/or carbonic diester; With
2) surfactant,
Wherein said compositions is foam state in use.
2. topical composition according to claim 1, it comprises:
1) effective ingredient;
2) N-alkyl-2-Pyrrolidone and/or carbonic diester; With
3) surfactant,
Wherein said compositions is foam state in use.
3. topical composition according to claim 2, wherein said effective ingredient comprises and is selected from following one or more: vitamin A and derivant, vitamin D and derivant thereof, vitamin E and derivant, immunosuppressant, antibiotic, antifungal, antiinflammatory, glucocorticoid, heparin and heparinoid.
4. the topical composition according to any one of claim 1-3, wherein said N-alkyl-2-Pyrrolidone comprises and is selected from following one or more: METHYLPYRROLIDONE, N-ethyl-2-pyrrolidone, N-propyl group-2-Pyrrolidone and N-butyl-2-Pyrrolidone.
5. the topical composition according to any one of claim 1-4, wherein said carbonic diester is propylene carbonate.
6. the topical composition according to any one of claim 1-5, wherein said surfactant comprises and is selected from following one or more: optionally add polyoxyethylated glycerine monofatty ester; The fatty acid ester of polyglycereol; The polyoxyethylated sorbitan fatty acid ester of optional interpolation; Polyoxyethylated alkyl ether or alkene ether; Fatty diglycollic amide; The polyoxyethylene castor oil be optionally hydrogenated.
7. the topical composition according to any one of claim 1-6, it comprises the alcohol being no less than 10 quality %.
8. topical composition according to claim 7, it comprises the glycerol being no less than 15 quality %.
9. the topical composition according to any one of claim 1-8, it forms foam with pump type foam maker in use.
10. by the topical composition according to any one of claim 2-9 being filled to the medicine prepared in pump type foam maker.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013-157134 | 2013-07-11 | ||
| JP2013157134 | 2013-07-11 | ||
| PCT/JP2014/068407 WO2015005419A1 (en) | 2013-07-11 | 2014-07-10 | External-use composition producing foamed state upon use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105392473A true CN105392473A (en) | 2016-03-09 |
| CN105392473B CN105392473B (en) | 2018-06-08 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN201480037345.2A Active CN105392473B (en) | 2013-07-11 | 2014-07-10 | The topical composition of foam state is generated during use |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11135297B2 (en) |
| EP (1) | EP3020392A4 (en) |
| JP (1) | JP6460988B2 (en) |
| KR (1) | KR20160030162A (en) |
| CN (1) | CN105392473B (en) |
| WO (1) | WO2015005419A1 (en) |
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| CN109310633A (en) * | 2016-06-16 | 2019-02-05 | 宝丽制药股份有限公司 | Foam, the composition and its evaluation method for sieving infusion |
| CN114828860A (en) * | 2019-03-05 | 2022-07-29 | 霍夫曼技术有限责任公司 | Transdermal microflora preparation |
| CN114848593A (en) * | 2022-05-30 | 2022-08-05 | 澳美制药厂有限公司 | Foam composition and preparation method thereof |
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| US9687528B2 (en) | 2014-12-23 | 2017-06-27 | Steven Hoffman | Transdermal formulations |
| AU2015371253B2 (en) * | 2014-12-23 | 2020-07-23 | Steven Hoffman | Transdermal formulations |
| JP2016121145A (en) * | 2014-12-24 | 2016-07-07 | 株式会社ポーラファルマ | External composition for screen foamer |
| JP6928760B2 (en) * | 2016-06-16 | 2021-09-01 | サンファーマ株式会社 | Foam, composition for screen formers, and how to evaluate them |
| JP2022532210A (en) | 2019-05-14 | 2022-07-13 | タイム，インコーポレーテッド | Compositions and Methods for Treating Cancer |
| US10905698B1 (en) | 2020-05-14 | 2021-02-02 | Tyme, Inc. | Methods of treating SARS-COV-2 infections |
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Also Published As
| Publication number | Publication date |
|---|---|
| US20160136278A1 (en) | 2016-05-19 |
| EP3020392A1 (en) | 2016-05-18 |
| JPWO2015005419A1 (en) | 2017-03-02 |
| KR20160030162A (en) | 2016-03-16 |
| CN105392473B (en) | 2018-06-08 |
| EP3020392A4 (en) | 2016-12-28 |
| WO2015005419A1 (en) | 2015-01-15 |
| US11135297B2 (en) | 2021-10-05 |
| JP6460988B2 (en) | 2019-01-30 |
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